Trimethylhydrazinium propionate

Pharmacological properties

the active substance of long-trizipine is trimethylhydrazinium propionate (meldonium) - a structural analogue of γ-butyrobetaine - a substance that is a precursor of carnitine. the drug, suppressing the activity of γ-butyrobetaine hydroxylase, reduces the biosynthesis of carnitine and the transport of long chain fatty acids to mitochondria, prevents the accumulation in the cells of activated forms of unoxidized fatty acids - derivatives of acylcarnitine a, thus preventing their adverse effects. Trisipine Long restores the balance of the processes of oxygen delivery and its consumption in cells; prevents the violation of the transport of atph, at the same time it activates glycolysis, which occurs without additional oxygen consumption. as a result of a decrease in carnitine concentration, γ-butyrobetaine, which has vasodilating properties, is intensely synthesized.

The mechanism of action of Trizipine Long determines a wide range of its pharmacological effects. Increases working capacity, reduces the severity of symptoms of mental and physical stress. The drug has a pronounced cardioprotective effect. With heart failure, it improves myocardial contractility, increases exercise tolerance. With stable angina II and III functional class increases the physical performance of patients and reduces the frequency of angina attacks.

In acute and chronic ischemic disorders of cerebral circulation, Trizipin Long improves blood circulation in the focus of ischemia, acting on the redistribution of cerebral blood flow in favor of the ischemic site. Trizipin Long also has a tonic effect on the central nervous system, eliminates functional disorders of the somatic and autonomic nervous system, including with withdrawal symptoms in patients with chronic alcoholism. The drug also has a positive effect on dystrophically altered retinal vessels and cellular immunity.

Pharmacokinetics The prolonged dosage form of Trizipin Long provides uniform release of the active substance with a release rate of 35–80 mg / h for different doses of Trizipin Long tablets regardless of pH level. WITH_max the active substance in the blood plasma is reached 5–6 hours after taking the drug and gradually decreases over the next 18–20 hours, remaining within the therapeutic range. The metabolism of trimethylhydrazinium propionate is carried out in the liver with the formation of two major metabolites that are excreted by the kidneys. T_½ is 15-17 hours

Indications

Trizipin long is used for therapeutic and prophylactic purposes as part of the complex therapy of coronary heart disease (angina pectoris, myocardial infarction, chronic heart failure, dishormonal cardiomyopathy); acute and chronic cerebrovascular accidents (cerebral strokes and chronic cerebrovascular insufficiency); hemophthalmus and retinal hemorrhages of various etiologies, thrombosis of the central retinal vein and its branches, retinopathy of various etiologies (diabetic, hypertensive). Trisipine Long is used for reduced performance, physical overload, including in sports practice, to accelerate the recovery of athletes, as well as with withdrawal symptoms and chronic alcoholism (in combination with specific therapy for alcoholism).

Application

Assign to adults inside, regardless of food intake. to ensure a gradual and uniform release of the active substance from the tablet, it should be swallowed whole with a glass of water.

In connection with the production technology of a prolonged form, along with feces, a soft spongy base is removed, which in shape resembles a tablet, but does not contain an active substance.

Doses of the drug Trizipin long should be selected individually in accordance with medical indications, the severity of the disease and the anatomical and physiological characteristics of the patients.

Cardiovascular disease or cerebrovascular accident. As part of complex therapy, up to 1.0 g / day in one dose. The course of treatment is 4-6 weeks.

Cardialgia on the background of dishormonal myocardial dystrophy - inside up to 1.0 g / day in one go. The course of treatment is 12 days.

The acute phase of cerebrovascular accident - up to 1.0 g / day in one go. The course of treatment is 4-6 weeks.

Chronic cerebrovascular accident - inside up to 1.0 g / day in one go. The course of treatment is 4-6 weeks. Repeated courses (usually 2-3 times a year) are possible after consultation with a doctor.

Vascular pathology and degenerative diseases of the retina. An injectable dosage form of the drug is used.

Mental and physical overload, including among athletes. Apply up to 2.0 g / day. The course of treatment is 10-14 days. If necessary, treatment is repeated after 2-3 weeks.

Athletes are prescribed up to 2.0 g / day before training. The duration of the course in the preparatory period is 14-21 days, during the competition period 10-14 days.

Chronic alcoholism Up to 2.0 g / day. The course of treatment is 7-10 days.

Contraindications

Hypersensitivity to any of the components of the drug. organic lesions of the central nervous system. increased intracranial pressure (with violations of the venous outflow, intracranial tumors), pregnancy, childhood.

Side effects

From the cardiovascular system: rarely - tachycardia, arrhythmia, changes in hell.

From the blood system: eosinophilia.

From the side of the central nervous system: rarely - headache, dizziness, psychomotor agitation, paresthesia, tremor, agitation.

From the digestive tract: rarely - diarrhea, nausea, vomiting, abdominal pain, dyspeptic symptoms, metallic taste in the mouth, dry mouth or hypersalivation.

Allergic reactions: rarely - redness and itching of the skin, urticaria, rash, angioedema; very rarely - anaphylactic shock.

From the respiratory system: shortness of breath, dry cough.

Other: chills, chest pain, weakness, hyperthermia, hyperhidrosis.

special instructions

The drug is used with caution in chronic diseases of the liver and kidneys. due to the possible development of a stimulating effect, it is recommended to take it in the morning.

Given the stimulating effect of Trizipine Long on sexual activity and potency, the drug should not be taken before bedtime. Since Trizipin Long inhibits the biosynthesis of carnitine, it should not be prescribed to patients with congenital carnitine deficiency, as well as patients with hyperthyroidism. Patients with severe arterial hyper- or hypotension are prescribed with caution, since isolated cases of abnormal reactions in such patients have been recorded. Patients with cirrhosis and severe renal impairment should not take Trizipine Long. This also applies to patients on hemodialysis, as a result of which the carnitine content is significantly reduced.

Due to the lack of comprehensive data on the safety and efficacy of trimethylhydrazinium propionate preparations for the treatment of children, Trizipine Long should not be prescribed to children under 12 years of age. The safety of the drug during pregnancy has not been conclusively proven. In order to avoid a possible negative effect on the formation of the fetus, Trizipin Long is not prescribed during pregnancy. Since the nature of the release of the drug into mother’s milk has not been finally clarified, in case of urgent need for treatment with Trizipine Long, breast-feeding is stopped for the duration of the drug.

In order to avoid the possible development of a stimulating effect, it is recommended to take Trizipine Long in the morning.

Use during pregnancy and lactation. Do not use.

Children. Not used in pediatric practice.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. During treatment, care must be taken when driving vehicles or working with other mechanisms, given the likelihood of side effects that can affect the speed of the reaction and the ability to concentrate.

Interactions

As part of complex therapy, Trisipine Long is used in combination with antianginal drugs, anticoagulants, antiplatelet agents, antiarrhythmic drugs, cardiac glycosides, diuretics, bronchodilators and other drugs. Trisipine Long can potentiate the effects of nitroglycerin, nifedipine, β-adrenergic blockers and peripheral vasodilators.

Overdose

Sudden changes in hell are possible. symptomatic therapy.

Storage conditions

In the original packaging at a temperature not exceeding 30 ° C.